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基于前体蛋白转化酶内源性和外源性抑制剂开发新型治疗药物的潜在机会。

Potential opportunity in the development of new therapeutic agents based on endogenous and exogenous inhibitors of the proprotein convertases.

作者信息

Bontemps Yannick, Scamuffa Nathalie, Calvo Fabien, Khatib Abdel-Majid

机构信息

INSERM, U 716, Equipe AVENIR, Institut de Génétique Moléculaire, Paris 75010, France.

出版信息

Med Res Rev. 2007 Sep;27(5):631-48. doi: 10.1002/med.20072.

Abstract

The proprotein convertases (PCs) are responsible for the endoproteolytic processing of various protein precursors (e.g., growth factors, receptors, adhesion molecules, and matrix metalloproteinases) implicated in several diseases such as obesity, diabetes, atherosclerosis, cancer, and Alzheimer disease. The potential clinical and pharmacological role of the PCs has fostered the development of various PC-inhibitors. In this review we summarized the recent findings on PCs inhibitors, their mode of actions and potential use in the therapy of various diseases.

摘要

前蛋白转化酶(PCs)负责多种蛋白质前体(如生长因子、受体、黏附分子和基质金属蛋白酶)的内切蛋白水解加工,这些蛋白质前体与肥胖、糖尿病、动脉粥样硬化、癌症和阿尔茨海默病等多种疾病有关。PCs的潜在临床和药理学作用推动了各种PC抑制剂的开发。在本综述中,我们总结了关于PC抑制剂的最新研究结果、它们的作用模式以及在各种疾病治疗中的潜在用途。

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